The present invention relates to novel mitomycin derivatives having anti-tumor and antibacterial activity.
Mitomycins are generally known to be antibiotics having antibacterial and anti-tumor activity. From natural sources, mitomycin C is mainly obtained and as trace components, mitomycin A, mitomycin B and porfiromycin (these are described in Merck Index, 10th edition) are obtained. Further, as trace components, there are also known mitomycins D and E (Japanese Published Unexamined Patent Application No. 122797/1979), mitomycins F and J (Japanese Published Unexamined Patent Application No. 45322/1980), mitomycins G, H and K (Japanese Published Unexamined Patent Application No. 118396/1980), and the like. Structures of these mitomycins obtained from natural sources are shown in Table 1.
TABLE 1 ______________________________________ Structures of mitomycins obtained from natural sources ##STR1## Mito- mycin X.sub.A Y.sub.A Z.sub.A R.sub.A R.sub.B ______________________________________ A OCH.sub.3 CH.sub.3 H CH.sub.2 OCONH.sub.2 H B OCH.sub.3 H CH.sub.3 H CH.sub.2 OCONH.sub.2 C NH.sub.2 CH.sub.3 H CH.sub.2 OCONH.sub.2 H D NH.sub.2 H CH.sub.3 H CH.sub.2 OCONH.sub.2 E NH.sub.2 CH.sub.3 CH.sub.3 H CH.sub.2 OCONH.sub.2 F OCH.sub.3 CH.sub.3 CH.sub.3 CH.sub.2 OCONH.sub.2 H G NH.sub.2 CH.sub.3 CH.sub.3 Combined together to form CH.sub.2 H OCH.sub.3 H CH.sub.3 Combined together to form CH.sub.2 J OCH.sub.3 CH.sub.3 CH.sub.3 H CH.sub.2 OCONH.sub.2 K OCH.sub.3 CH.sub.3 CH.sub.3 Combined together to form CH.sub.2 Porfiro- NH.sub.2 CH.sub.3 CH.sub.3 CH.sub.2 OCONH.sub.2 H mycin ______________________________________
Some of the above mitomycins show an excellent anti-tumor activity, but they have also serious side effects such as decrease in leucocytes, etc. In view of such background, many derivatives have been synthesized to enhance the activity or to alleviate the toxicity
Concerning compounds wherein the C.sub.6 -methyl group is modified and which are relevant to the present invention, an application directed to mitomycin derivatives of general formula (I) later described wherein W is deuterium (.sup.2 H) or tritium (.sup.3 H) was filed by the present applicant [Japanese Patent Application No. 227094/1987 (Japanese Published Unexamined Patent Application No. 70490/1989)].